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At least 127 records · Page 7Linked to original sources
PubMed1991

Lecithin: cholesterol acyltransferase activity in familial hypercholesterolemia treated with simvastatin and simvastatin plus low-dose colestipol.

In 19 patients with heterozygous familial hypercholesterolemia (FH), the effects of simvastatin (S) 20 mg/d, 40 mg/d, and 40 mg/d plus low-dose colestipol (10 g/d) on plasma lipids, plasma lipoproteins, and plasma lecithin: cholesterol acyltransferase (LCAT) activity were investigated after an original dose-range escalation/descalation design. The drug regimen was changed every 8 weeks. A significant reduction in total cholesterol and LDL-cholesterol was observed, reaching 39% and 54% for the drug combination (week 28), and total apoprotein B and LDL-apoprotein B were reduced by 39% and 50%, respectively. Triglycerides were significantly lowered by S alone (up to 29% with 40 mg/d). HDL-cholesterol increased during therapy but the cholesterol content in HDL2-HDL3 fractions (isolated by ultracentrifugation) did not change significantly during the different steps. The ratio LDL-C/HDL-C fell by 57% at week 28. Plasma LCAT activity expressed as FER was significantly enhanced by S alone (+33%), and a further increase on drug combination regimen (+58%) was observed. This effect could be considered as a consequence of the increased fractional clearance of LDL-C. It tended to be sustained during the descalation part of the study. Biochemical adverse effects were scarce and transient. In conclusion, the combination therapy increased the plasma LCAT/FER activity without a preferential enhancement in HDL2-C concentration. This original design allowed to define the most appropriate individual cholesterol-lowering drug dosage in FH patients.

Adolescent↗
PubMed1983

The effects of cholestyramine, colestipol, and ADR-132 on the rat prostate and dunning R-3327 adenocarcinoma.

The effects of three compounds known to have hypocholesterolemic activity in several species were investigated on the rat prostate and the hormone-dependent R-3327 rat prostatic adenocarcinoma. Cholestyramine, colestipol, and ADR-132 are bile acid-sequestering anion exchange resins which were fed to separate groups of adult male Copenhagen X Fischer (F1) hybrid rats in doses of 0.25%, 1.00%, and 2.00% of diet. The results indicate that serum cholesterol levels in tumor-bearing rats and controls fed these compounds for 29 days were not reduced. The body and organ weights as well as the histological features of the prostate gland, seminal vesicles, and the R-3327 tumor were unaffected by these agents.

Adenocarcinoma↗
PubMed1983

Effect of cholestyramine and colestipol on the absorption of phenytoin.

The hypocholesterolemic cation resins, cholestyramine and colestipol, have variable effects on the absorption parameters of a number of lipophillic, anion drugs. Because of the unpredictable nature of this interaction, we have assessed in human volunteers the effect of these resins on the rate and total absorption of phenytoin. Our results indicate that these resins do not affect the absorption parameters of phenytoin and that special care does not have to be exercised when these agents are co-administered.

Adolescent↗
PubMed1993

Hypocholesterolemic effects of cholestyramine and colestipol in patients with familial defective apolipoprotein B-100.

Familial defective apolipoprotein B-100 (FDB) is a dominantly inherited disorder associated with hypercholesterolemia, in which substitution of the amino acid glutamine for arginine at position 3500 in the apoprotein B molecule results in LDL particles which bind poorly to the LDL receptor. To date, patients with FDB have been heterozygous for this disorder and their plasma contains both normal and defective-binding LDL particles, with a predominance of the latter. In the present report, we have compared the hypocholesterolemic effects of bile acid sequestrant therapy (cholestyramine or colestipol) in eight patients with FDB, to the response seen in sixteen patients with heterozygous familial hypercholesterolemia (FH), treated with the same drugs. Concentrations of LDL cholesterol fell by 32.0% in the patients with FDB and by 21.6% in the patients with FH. The results indicate that the hypercholesterolemia of both FDB and FH responds to treatment with bile acid sequestrants.

Adult↗
PubMed1997

Moderate dose, three-drug therapy with niacin, lovastatin, and colestipol to reduce low-density lipoprotein cholesterol <100 mg/dl in patients with hyperlipidemia and coronary artery disease.

The efficacy, safety, and tolerability of a moderate dose, 3-drug lipid-lowering regimen were evaluated among 29 male patients with hyperlipidemia and coronary artery disease. In an initial 12-month phase, regular niacin, 500 mg qid, lovastatin, 20 mg bid, and colestipol, 10 g/bid, were given with dose adjustment for lipid targets and side effects. This was followed by 2 random sequence crossover phases (8 months each) alternating regular niacin with a polygel controlled-release formulation of niacin for use in this regimen. Lipid, lipoprotein, apoprotein, and clinical chemistry determinations were obtained at baseline, during the initial phase, at the 2 crossover phases, and at 6 weeks after therapy. A final questionnaire queried specific side effects and overall preferences. Low-/high-density lipoprotein (LDL/HDL) changed from means of 215/46 mg/dl at baseline, to 94/59 mg/dl after run-in, to 85/52 mg/dl after 8 months of controlled-release niacin, and to 98/56 mg/dl after 8 months of regular niacin (regular niacin vs controlled-release niacin, p <0.005/<0.05). The target of LDL < or = 100 mg/dl was achieved at 8 months by 83% of these patients with controlled-release niacin and by 52% with regular niacin (p <0.01). Compliance was 95% with controlled-release niacin versus 85% with regular niacin (p <0.001). The controlled-release niacin and regular niacin regimens did not differ in terms of uric acid, glucose, insulin, or asparate aminotransferase levels. Overall, 21% of patients called the 3 drugs "very easy" and 72% "fairly easy" to take. The controlled-release niacin-containing regimen was preferred by 21 patients and the regular niacin by 4. In conclusion, these regimens achieve striking lipid changes among hyperlipidemic patients. Controlled release is the preferred niacin preparation in terms of LDL reduction, compliance, patient preference, and achieving the National Cholesterol Education Program guideline of LDL < or = 100 mg/dl. The 2 niacin preparations did not differ in evidence of toxicity.

Cholesterol, LDL↗
PubMed1986

Enhanced withdrawal from chickens of hexachlorobenzene (HCB) and pentachlorophenol (PCP) by colestipol, mineral oil, and/or restricted feeding.

Young chickens fed hexachlorobenzene (HCB) or pentachlorophenol (PCP) for 14 d at 10 ppm in the diet contained body burdens of 573 or 362 micrograms, respectively. These diets were withdrawn (d 0) and replaced for 21 d with diets containing 5% mineral oil (MO), or 5% colestipol (CO), a bile-acid-binding resin, or the chickens were restricted in feed intake to 50% of controls (50-RF), fed MO plus 50-RF, or CO plus 50-RF. Without any treatment during withdrawal, body burdens were reduced to 63% and 70% of the d 0 values for HCB and PCP, respectively. MO, CO, or 50-RF reduced body burdens of HCB to 37% of d 0 burdens, but the combination treatments with 50-RF reduced body burdens to 19% of d 0 values. PCP was at 35% of the d 0 burdens from 50-RF, while all other treatments had reduced body burdens to nondetectable amounts of less than 0.7 micrograms/bird by d 21 of withdrawal. Body fat was not reduced by mineral oil, but was reduced to some extent by CO, and was markedly reduced by 50-RF. 50-RF always reduced body burdens of PCP or HCB alone or in combination with MO or CO. These data are discussed in relationship to the nonbiliary excretion of xenobiotics.

Adipose Tissue↗
PubMedDate not supplied

Combined therapy of niacin, colestipol, and fat-controlled diet in men with coronary bypass. Effect on blood lipids and apolipoproteins.

The effects of colestipol (30 grams/day), niacin (7.3 grams/day), and diet on blood lipids and apolipoproteins after one year of therapy are reported. Men selected on the basis of previous coronary artery bypass surgery were randomly assigned to drug or control treatments in an angiographic study of atherosclerosis progression and regression. In 14 men, drugs and diet produced the following changes: Baseline total cholesterol 245 mg/dl, triglyceride 189 mg/dl, and LDL cholesterol 164 mg/dl were decreased by 73 mg/dl (29%), 83 mg/dl (41%) and 69 mg/dl (40%) respectively. Baseline HDL cholesterol, 44 mg/dl was increased 13 mg/dl (33%). Baseline apolipoprotein B, 124 mg/dl and apolipoprotein C-III (heparin precipitate) 5.6 mg/dl were decreased 40 mg/dl (31%) and 2.4 mg/dl (41%) respectively. All these changes are significant, p less than 0.01. Apolipoprotein A-I and apolipoprotein C-III (heparin supernate) were not significantly changed. In the controls, placebo and diet produced no significant decrease in blood lipid or lipoproteins, with the exception that baseline apolipoprotein B, 111 mg/dl increased 18 mg/dl (12%), p less than 0.05.

Adult↗
PubMed1991

Effects of colestipol-niacin therapy on human femoral atherosclerosis.

The 2-year therapy effect on femoral atherosclerosis was evaluated in the Cholesterol Lowering Atherosclerosis Study (CLAS), a randomized, placebo-plus-diet-controlled angiographic trial of colestipol-niacin therapy plus diet in men with previous coronary bypass surgery. Different diet compositions were prescribed to enhance the differential in blood cholesterol responses between the two groups. The annual rate of change in computer-estimated atherosclerosis (CEA), a measure of lumen abnormality, was evaluated between treatment groups. A significant per-segment therapy effect was found in segments with moderately severe atherosclerosis (p less than 0.04) and in proximal segments (p less than 0.02). When segmental CEA measures were combined into a per-patient score using an adaptation of the National Heart, Lung, and Blood Institute scoring procedure, a significant therapy effect was observed (p less than 0.02). Total variance of the annual change rate in CEA was as predicted from pilot studies, but measurement variation was larger. The therapy effect observed in femoral arteries, although significant, was less marked than the strong and consistent benefit previously reported for both native coronary arteries and aortocoronary bypass grafts.

Arteriosclerosis↗
PubMedDate not supplied

Extracranial carotid arterial disease in patients with familial hypercholesterolemia and coronary artery disease treated with colestipol and nicotinic acid.

Carotid bifurcation atherosclerosis was demonstrated in 34 of 108 patients with familial hypercholesterolemia and coronary artery disease by B-scan, continuous-wave Doppler sonography, and intravenous digital subtraction angiography. An intensive combined therapy of diet, colestipol, and nicotinic acid was mounted to control the hypercholesterolemia of these patients. Their serial sonographies and digital subtraction angiography were evaluated independently by technical specialists who served as coinvestigators. The data obtained suggest that extracranial arterial disease can develop concurrently with coronary artery disease in a significant proportion of patients with familial hypercholesterolemia, and amaurosis fugax, transient ischemic attack, cerebral infarction, and myocardial infarction did not recur during 58-72 months of control of familial hypercholesterolemia in this series of patients.

Adult↗
PubMed1989

Enhanced withdrawal of polychlorinated biphenyls: a comparison of colestipol, mineral oil, propylene glycol, and petroleum jelly with or without restricted feeding.

Meat type chickens were fed a commercial mixture of polychlorinated biphenyl (PCB), Aroclor 1254, at 10 ppm for 14 days, then treated for 21 days to hasten the withdrawal of PCB with either mineral oil (MO), petroleum jelly (PJ), propylene glycol (PG), or colestipol (CO) at 5% of the diet, or at 10% of the diet when restricted to 50% of control intake (50% FR). Whole carcass analyses for PCB revealed that MO + 50% FR reduced PCB to 1.91 mg/bird, or 32% of the body burden (5.96 mg) in nontreated chickens previously fed PCB, whereas those restricted in feed intake by 50% (50% FR) had almost no change (6.44 mg/bird) in body burdens. The PJ, PG, and CO in combination with 50% FR reduced body burdens of PCB to 47, 57, and 77%, respectively, of the control value. When treated with MO, PJ, PG, or CO alone (no 50% FR), chickens had body burdens reduced to only 67 to 90% of control, depending on th compound. Thus, feed restriction was necessary for the MO and PJ to have their greatest effect. Carcass lipid values and body weight gains were markedly reduced by the feed restriction. The CO reduced carcass lipid in nonrestricted chickens by 30%.

Animal Feed↗
PubMed1990

Beneficial effects of colestipol-niacin on coronary atherosclerosis. A 4-year follow-up.

The Cholesterol Lowering Atherosclerosis Study (CLAS) was a randomized, placebo-controlled, angiographic trial testing combined colestipol-niacin therapy in 162 subjects. Two-year results (CLAS-I) showed decreased atherosclerosis progression and increased regression. We now describe a subgroup of 103 subjects treated for 4 years (CLAS-II). Changes in blood lipid, lipoprotein-cholesterol, and apolipoprotein levels were maintained, and at 4 years significantly more drug-treated subjects demonstrated nonprogression (52% drug- vs 15% placebo-treated) and regression (18% drug- vs 6% placebo-treated) in native coronary artery lesions. Significantly fewer drug-treated subjects developed new lesions in native coronary arteries (14% drug- vs 40% placebo-treated) and bypass grafts (16% drug- vs 38% placebo-treated). These results confirm CLAS-I findings and indicate that regression can continue for 4 years. They reaffirm the need for early initiation of vigorous long-term lipid lowering therapy in coronary bypass subjects.

Adult↗
PubMed1987

Treatment of primary moderate hypercholesterolemia with lovastatin (mevinolin) and colestipol.

The introduction of inhibitors of cholesterol biosynthesis offers a new approach to treatment of hypercholesterolemia. One such agent, lovastatin (formerly, mevinolin), causes significant reductions in plasma cholesterol levels. This action can be enhanced by bile acid sequestrants. In this study, lovastatin and colestipol hydrochloride together were administered to ten patients with primary moderate hypercholesterolemia. Compared with a control period, the combined-drug therapy caused a 36% reduction in plasma total cholesterol level, a 48% decrease in low-density lipoprotein (LDL) cholesterol level, and a 17% increase in high-density lipoprotein cholesterol level. The reduction in LDL cholesterol level was due to three factors: a 27% decrease in the production rate of LDL, a 20% increase in fractional catabolic rate of LDL, and a 15% depletion of cholesterol in LDL particles. This major reduction in LDL cholesterol level produced by combined-drug therapy may be valuable for prevention of coronary heart disease in high-risk patients with primary moderate hypercholesterolemia.

Aged↗
PubMed1979

In vitro binding of various biological substances by two hypocholesterolaemic resins. Cholestyramine and colestipol.

The ability of cholestyramine and colestipol, two hypocholesterolaemic resins, to bind in vitro several compounds such as vitamin B12, vitamin B12-intrinsic factor complex, folic acid, iron citrate and calcium chloride was investigated. Both resins bound to a high extent vitamin B12-intrinsic factor complex, folic acid and iron citrate; in addition, cholestyramine also caused appreciable binding of calcium. Throughout a large range of pH, there was no change in the binding capacity; however, at pH 2, cholestyramine exhibited a marked drop in the binding of tested substances (with exception of folic acid). By increasing the molarity of the solutions, the binding to the resins of vitamin B12-intrinsic factor complex and of calcium chloride was completely inhibited. In human gastric and duodenal juices, the uptake by the resins of the studied compounds depends on the molarity of the physiological medium tested and partly confirms the results obtained with aqueous solutions. These data obtained in vitro emphasize the necessity of regular monitoring these biochemical parameters during chronic treatment of hypercholesterolaemia conducted with these two resins.

Body Fluids↗
PubMed1981

[Long-term therapy of hypercholesteremia in diabetics with colestipol].

64 hypercholesterolemic diabetics (17 males and 47 females) were treated with Colestipol for 3 years. An average reduction of 29% in serum cholesterol levels was observed after 3 years. An increase in triglyceride levels was observed in several instances. Other laboratory data failed to reveal any deviation from normal ranges. Gastrointestinal complaints and constipation were initially noted with onset of therapy. These side effects resolved with continuation of treatment.

Aged↗
PubMed1985

[Long-term therapy of familial hypercholesterolemia in young patients with colestipol: availability of minerals and vitamins].

Longterm treatment for 5 years of young patients with familial hypercholesterolemia was accompanied by monitoring of plasma levels of calcium, iron, sodium, parathyroid hormone and water- and fat soluble vitamins, since interference of the ion exchange resin with absorption of numerous substances as well as abnormal plasma levels of some of the above had been described in several studies. Treatment was effective in the group with good compliance (lowering of plasma cholesterol at the end of 5 years by 19% and, compared to the control group, by 23%). Adverse drug effects with respect to the above parameters were not found. Plasma levels of carotinoides and vitamin E were elevated in the patients according to elevated concentrations of lipoproteins which are carriers of these vitamins.

Adolescent↗